Departments of Molecular Biology and Biochemistry, Pharmaceutical Sciences, and Chemistry, University of California, Irvine, CA 92697-3900.
Proc Natl Acad Sci U S A. 2013 Nov 5;110(45):18127-31. doi: 10.1073/pnas.1314080110. Epub 2013 Oct 21.
Nitric oxide (NO) produced by bacterial NOS functions as a cytoprotective agent against oxidative stress in Staphylococcus aureus, Bacillus anthracis, and Bacillus subtilis. The screening of several NOS-selective inhibitors uncovered two inhibitors with potential antimicrobial properties. These two compounds impede the growth of B. subtilis under oxidative stress, and crystal structures show that each compound exhibits a unique binding mode. Both compounds serve as excellent leads for the future development of antimicrobials against bacterial NOS-containing bacteria.
一氧化氮(NO)由细菌 NOS 产生,可作为金黄色葡萄球菌、炭疽芽孢杆菌和枯草芽孢杆菌对抗氧化应激的细胞保护剂。对几种 NOS 选择性抑制剂的筛选发现了两种具有潜在抗菌特性的抑制剂。这两种化合物在氧化应激下抑制枯草芽孢杆菌的生长,晶体结构表明,每种化合物都表现出独特的结合模式。这两种化合物都可以作为开发针对含有细菌 NOS 的细菌的抗菌药物的优秀先导化合物。